Id: acc2015
Group: 2sens
Protein: KIT
Gene Symbol: KIT
Protein Id: P10721
Protein Name: KIT_HUMAN
PTM: phosphorylation
Site: Tyr703
Site Sequence: QEDHAEAALYKNLLHSKESSC
Disease Category: Cancer
Disease: Lung Cancer
Disease Subtype: NSCLC KITD816G
Disease Cellline: HCC78
Disease Info:
Drug: ponatinib
Drug Info: "Ponatinib is a third-generation tyrosine kinase inhibitor approved for the treatment of chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL), particularly in patients with the T315I mutation or resistance to prior tyrosine kinase inhibitor therapies, with a boxed warning for vascular occlusion, thrombosis, heart failure, and hepatotoxicity."
Effect: modulate
Effect Info: Drug inhibits protein phosphorylation
Note: no tumor effct
Score: 3.0
Pubmed(PMID): 27068398
Sentence Index:
Sentence:

Sequence & Structure:

MRGARGAWDFLCVLLLLLRVQTGSSQPSVSPGEPSPPSIHPGKSDLIVRVGDEIRLLCTDPGFVKWTFEILDETNENKQNEWITEKAEATNTGKYTCTNKHGLSNSIYVFVRDPAKLFLVDRSLYGKEDNDTLVRCPLTDPEVTNYSLKGCQGKPLPKDLRFIPDPKAGIMIKSVKRAYHRLCLHCSVDQEGKSVLSEKFILKVRPAFKAVPVVSVSKASYLLREGEEFTVTCTIKDVSSSVYSTWKRENSQTKLQEKYNSWHHGDFNYERQATLTISSARVNDSGVFMCYANNTFGSANVTTTLEVVDKGFINIFPMINTTVFVNDGENVDLIVEYEAFPKPEHQQWIYMNRTFTDKWEDYPKSENESNIRYVSELHLTRLKGTEGGTYTFLVSNSDVNAAIAFNVYVNTKPEILTYDRLVNGMLQCVAAGFPEPTIDWYFCPGTEQRCSASVLPVDVQTLNSSGPPFGKLVVQSSIDSSAFKHNGTVECKAYNDVGKTSAYFNFAFKGNNKEQIHPHTLFTPLLIGFVIVAGMMCIIVMILTYKYLQKPMYEVQWKVVEEINGNNYVYIDPTQLPYDHKWEFPRNRLSFGKTLGAGAFGKVVEATAYGLIKSDAAMTVAVKMLKPSAHLTEREALMSELKVLSYLGNHMNIVNLLGACTIGGPTLVITEYCCYGDLLNFLRRKRDSFICSKQEDHAEAALYKNLLHSKESSCSDSTNEYMDMKPGVSYVVPTKADKRRSVRIGSYIERDVTPAIMEDDELALDLEDLLSFSYQVAKGMAFLASKNCIHRDLAARNILLTHGRITKICDFGLARDIKNDSNYVVKGNARLPVKWMAPESIFNCVYTFESDVWSYGIFLWELFSLGSSPYPGMPVDSKFYKMIKEGFRMLSPEHAPAEMYDIMKTCWDADPLKRPTFKQIVQLIEKQISESTNHIYSNLANCSPNRQKPVVDHSVRINSVGSTASSSQPLLVHDDV

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
KIT DASATINIB Stem cell growth factor receptor inhibitor 4 - acute lymphoblastic leukemia DailyMed
DailyMed
KIT DASATINIB Stem cell growth factor receptor inhibitor 4 Unknown status acute lymphoblastic leukemia ClinicalTrials
KIT MIDOSTAURIN Stem cell growth factor receptor inhibitor 4 - acute myeloid leukemia FDA
KIT DASATINIB Stem cell growth factor receptor inhibitor 4 - chronic myelogenous leukemia DailyMed
DailyMed
KIT DASATINIB Stem cell growth factor receptor inhibitor 4 Completed chronic myelogenous leukemia ClinicalTrials
ClinicalTrials
KIT IMATINIB MESYLATE Stem cell growth factor receptor inhibitor 4 - chronic myelogenous leukemia DailyMed
DailyMed
KIT DASATINIB Stem cell growth factor receptor inhibitor 4 Recruiting chronic myelogenous leukemia ClinicalTrials
ClinicalTrials
ClinicalTrials
KIT DASATINIB Stem cell growth factor receptor inhibitor 4 Unknown status chronic myelogenous leukemia ClinicalTrials
KIT IMATINIB MESYLATE Stem cell growth factor receptor inhibitor 4 Completed chronic myelogenous leukemia ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
KIT SUNITINIB Stem cell growth factor receptor inhibitor 4 Completed neoplasm ClinicalTrials
KIT DASATINIB Stem cell growth factor receptor inhibitor 4 - neoplasm ATC
KIT MIDOSTAURIN Stem cell growth factor receptor inhibitor 4 - neoplasm ATC
KIT MASITINIB Stem cell growth factor receptor inhibitor 4 - neoplasm ATC
KIT REGORAFENIB Stem cell growth factor receptor inhibitor 4 - neoplasm ATC
KIT PEXIDARTINIB Stem cell growth factor receptor inhibitor 4 - neoplasm ATC
KIT AVAPRITINIB Stem cell growth factor receptor inhibitor 4 - neoplasm ATC
KIT RIPRETINIB Stem cell growth factor receptor inhibitor 4 - neoplasm ATC
KIT SUNITINIB Stem cell growth factor receptor inhibitor 4 - neoplasm ATC
KIT SUNITINIB Stem cell growth factor receptor inhibitor 4 Completed renal cell carcinoma ClinicalTrials
ClinicalTrials
KIT SUNITINIB Stem cell growth factor receptor inhibitor 4 Terminated renal cell carcinoma ClinicalTrials
ClinicalTrials
KIT PAZOPANIB HYDROCHLORIDE Stem cell growth factor receptor inhibitor 4 - renal cell carcinoma DailyMed
FDA
KIT SUNITINIB MALATE Stem cell growth factor receptor inhibitor 4 Completed renal cell carcinoma ClinicalTrials
KIT SORAFENIB TOSYLATE Stem cell growth factor receptor inhibitor 4 - renal cell carcinoma DailyMed
KIT PAZOPANIB HYDROCHLORIDE Stem cell growth factor receptor inhibitor 4 - sarcoma DailyMed
FDA
KIT SUNITINIB MALATE Stem cell growth factor receptor inhibitor 4 - renal cell carcinoma DailyMed

Note: Only show clinically investigational or approved drugs with protein targets.

Protein Tractability:

source: Open Targets
Small molecule
Antibody
PROTAC
Other modalities
Approved Drug
Advanced Clinical
Phase 1 Clinical
Structure with Ligand
High-Quality Ligand
High-Quality Pocket
Med-Quality Pocket
Druggable Family
Approved Drug
Advanced Clinical
Phase 1 Clinical
UniProt loc high conf
GO CC high conf
UniProt loc med conf
UniProt SigP or TMHMM
GO CC med conf
Human Protein Atlas loc
Approved Drug
Advanced Clinical
Phase 1 Clinical
Literature
UniProt Ubiquitination
Database Ubiquitination
Half-life Data
Small Molecule Binder
Approved Drug
Advanced Clinical
Phase 1 Clinical

PTM Intensity:

source: CPTAC
KIT-Tyr703
Cancer Intensity
BRCA
COAD
HGSC
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
Y 703 U Gastrointestinal stromal tumor Phosphorylation 15007386

State Note: Based on the distinct PTM states in diseases, PTMD classified all disease-associated PTMs into six classes, including whether the up-regulation (U) or down-regulation (D) of PTM levels, the absence (A) or presence (P) of PTMs, and the creation (C) or disruption (N) of PTM sites are associated with diseases.

PTM-Drug Perturbation Response:

source: DecryptM

No data.

Function score:

source: funscoR

No data.

Cross Links: